Synthesis andin vitro antibacterial activity of quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety

Several oxazolidinones having amine moiety were prepared to form a quaternary ammonium salt with cephalosporin nucleus, and antibacterial activity of the quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety were examined particularly with expectation of dual activity. However, the cephalosporin-oxazolidinone compounds revealed rather weaker antibacterial activity in vitro than their parent oxazolidinone and cephalosporin without showing any characteristic activity as expected.     

Emergence of ceftriaxone-resistant Salmonella isolates and rapid spread of plasmid-encoded CMY-2-like cephalosporinase,Taiwan

Of 384 Salmonella isolates collected from 1997 to 2000 in a university hospital in Taiwan, six ceftriaxone-resistant isolates of Salmonella enterica serovar Typhimurium were found in two patients in 2000. The resistance determinants were on conjugative plasmids that encoded a CMY-2-like cephalosporinase. During the study period, the proportion of CMY-2-like enzyme producers among Escherichia coli increased rapidly from 0.2% in early 1999 to >4.0% in late 2000. Klebsiella pneumoniae isolates producing a CMY-2-like beta-lactamase did not emerge until 2000. The presence of bla(CMY)-containing plasmids with an identical restriction pattern from Salmonella, E. coli, and K. pneumoniae isolates was found, which suggests interspecies spread and horizontal transfer of the resistance determinant. Various nosocomial and community-acquired infections were associated with the CMY-2-like enzyme producers. Our study suggests that the spread of plasmid-mediated CMY-2-like beta-lactamases is an emerging threat to hospitalized patients and the public in Taiwan.     

Thrombotic thrombocytopenic purpura in a postoperative patient taking cephalexin responding to plasmapheresis: A case report and review of cephalosporin‐induced TTP

The clinical presentation of thrombotic thrombocytopenic purpura (TTP) is often atypical delaying diagnosis and treatment. A number of drugs have been implicated in the development of TTP, including cyclosporine, tacrolimus, clopidogrel, and quinine. To our knowledge, only three cases of cephalosporin‐induced TTP have been described, with two of these cases occurring with these use of cephalexin. We herein describe a case of TTP occurring in a postoperative patient taking cephalexin, requiring plasmapheresis. Following plasmapheresis, the patient's mental status and platelet count significantly improved. J. Clin. Apheresis 31:473–475, 2016. © 2015 Wiley Periodicals, Inc.     

Antimicrobial Activity of Ro 41-1879, a New Catechol Cephalosporin

Summary

The antimicrobial activity and spectrum of Ro 41-1879, a new 7’-catcchol substituted cephalosporin, was assessed in a broth microdilution system against 312 clinical isolates. Ro 41-1879 demonstrated a slightly superior spectrum of activity (2- to 32-fold) compared to ceftazidime against Gram-positive cocci, Pscudotnonas spp. and Xanthomonas maltophilia. Enterobacteriaceae strains were more susceptible (97% versus 96%) to ceftazidime at S16 ≤ μg/ml. These results represent a preliminary potency/spectrum analysis for Ro 41-1879 since the screening studies were performed with an in vitro system unlikely to detect the potency contributed by active drug transport (tonB system) into bacterial cells. This new class of cephalosporins shows some therapeutic promise.     

Clinical outcomes of keratitis

OBJECTION: To analyse the patient, clinical and microbiological variables associated with poor outcomes from keratitis in patients presenting to a major public hospital in Australia. METHODS: A retrospective audit of the records of all patients who had a corneal scraping in 5 years at Princess Alexandra Hospital (Brisbane, Australia) was carried out. The outcome of a patient's episode of keratitis was classified as poor if they had final visual acuity of 6/60 or worse; had vision loss during treatment; or a complication of keratitis; or needed surgical intervention. RESULTS: A final outcome was established in 207 cases during the 5-year period. Final vision of 6/12 or better was found in 48% (100) of cases while a poor outcome was seen in 28% (58). Linear regression showed poor outcomes were directly associated with age (P < 0.001) and disease severity (P < 0.001). Univariate analysis indicated that poor outcomes were more likely in patients who had had prior ocular surgery (P = 0.005) or ocular surface disease (P = 0.01) and were also associated with presenting visual acuity of worse than 6/60 (P < 0.001) and isolation of Streptococcus pneumoniae (P = 0.002). While patients with traumatic keratitis, contact lens-related keratitis or negative corneal cultures (P = 0.009) were more likely to have good outcomes. Multivariate analysis showed that the relative risk of a patient having a poor outcome was 4.3x (CI 2.0-9.5) if they had severe keratitis, 4.1x (CI 1.8-9.5) if they had keratitis related to ocular surface disease and 3.8x (CI 1.8-8.3) if they were over 50 years old. CONCLUSIONS: An outcome of poor vision, vision loss during treatment, surgical intervention or complication of keratitis is more likely in patients with severe keratitis, keratitis related to prior ocular surface disease or older age.     

3—碘代甲基头孢菌素重要中间体GIE的合成

报道了由头孢菌素重要活性中间体GCLE制备GIE的有效方法,采用HPLC跟踪反应,摸索了最佳反应条件,操作简单,收率高于95％。     

部份降解的头孢噻肟酸转钠结晶工艺

目的：从部份降解的头孢噻肟酸回收头孢噻肟钠。方法：部份降解的头孢噻肟酸与醋酸钠反应后。加入吸附剂吸附降解杂质,再将反应液加入有机溶剂析出头孢噻肟钠。结果：得到合格的头孢噻肟钠。     

Emerging cephalosporins

Several cephalosporins are in clinical development as broad-spectrum agents with potent activity against multi-resistant staphylococci as well as the Gram-positive and Gram-negative bacteria normally susceptible to advanced generation cephalsoporins. These agents represent a novel activity for the class and challenge a dogma that β-lactams do not have clinically useful activity against multi-resistant staphylococci. The most advanced of these agents, ceftobiprole, is approaching registration and, if approved, will present physicians with a new paradigm in treatment of serious infections by multi-resistant organisms.     

Penetration of Cefonicid into Serum,Salpinges, Cervix and Vaginal Tissue

Summary

Cefonicid is a new cephalosporin that, given in adequate concentrations is able to kill some pathogens such as Grampositive cocci and many Enterobacteriaceae. In this study we have evaluated 40 patients receiving 1 g of cefonicid i.m. at various times before abdominal or vaginal hysterectomy. The results of the present study indicate that a single dose of 1 g of cefonicid given intramuscularly is useful as prophylaxis and treatment of gynecological infections.     

7－（香豆素－3－甲酰胺）－3－［1－（取代）吡啶基甲基］头孢菌素的合成

目的：探讨３＇－乙酰氧基被Ｎ－亲核试剂取代的反应条件、分离精制方法和新头孢菌素的体外抗菌活性。方法：７－（香豆素－３－甲酰胺）头孢菌素在ＮａＩ或ＫＳＣＮ的存在下与吡啶和β－甲基吡啶反应，产物用大孔吸附树脂及葡聚糖凝胶柱层析分离。结果：合成的二个新头孢菌素化合物，由红外光谱、元素分析和核磁共振谱确证其化学结构。体外抗菌试验表明，对某些革兰阴性菌有一定的抑菌作用。结论：该反应中加入大量的ＮａＩ可缩短反应时间并减少杂质。大孔吸附树脂可有效地将头孢菌素与无机盐分离。